1139-83-9Relevant articles and documents
Design, synthesis, and biological evaluation of novel 6h-benzo[c]chromen-6-one derivatives as potential phosphodiesterase ii inhibitors
Tang, Long,Jiang, Jianchun,Song, Guoqiang,Wang, Yajing,Zhuang, Ziheng,Tan, Ying,Xia, Yan,Huang, Xianfeng,Feng, Xiaoqing
, (2021/05/29)
Urolithins (hydroxylated 6H-benzo[c]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6H-benzo[c]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6H-benzo[c]chromen-6-one derivative 1f was found to have the optimal inhibitory potential (IC50: 3.67 ± 0.47 μM). It also exhibited comparable activity in comparison to that of BAY 60-7550 in vitro cell level studies.
Urolithin compound, preparation method, pharmaceutical composition and application
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Paragraph 0066-0075, (2021/09/04)
The invention belongs to the field of medicinal chemistry, and particularly relates to a urolithin compound, a preparation method, a pharmaceutical composition and application. The urolithin compound is a compound as shown in a general formula I or an optical isomer, an enantiomer, a diastereomer, a raceme or a raceme mixture of the compound, or a pharmaceutically acceptable salt of the compound. The urolithin compound provided by the invention has good PDE2 inhibitory activity, the enzymatic level IC50 reaches 3.67 [mu] M, and the urolithin compound can be used for treating central nervous system diseases and brain neurodegenerative process diseases, and can be used as an active component to prepare drugs for inhibiting PDE2 activity.
3-Hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-6H-benzo[c] chromen-6-one act as on-off selective fluorescent sensors for Iron (III) under in vitro and ex vivo conditions
FALLAH, Amirhossein,GüLCAN, Hayrettin Ozan,GAZI, Mustafa,KALKAN, Rasime,SHUKUR, Karar,TERALI, Kerem
, p. 858 - 867 (2021/07/26)
Regarding the abundant use of metals for different purposes, it becomes more critical from various scientific and technological perspectives to discover novel agents as selective probes for the detection of specific metals. In our previous studies, we have shown that aqueous solutions of natural urolithins (i.e., hydroxyl-substituted benzo[c]chromen-6-one derivatives) are selective Iron (III) sensors in fluorescence assays. In this study, we have extrapolated these findings to another coumarine compound (i.e., 3-Hydroxy-7,8,9,10- tetrahydro-6H-benzo[c]chromen-6-one) and compared the selective metal binding properties with Urolithin B (i.e., 3-Hydroxy-6H-benzo[c]chromen-6-one). Following the synthesis and structure identification studies, the fluorometric studies pointed out that the lactam group in the structure still persists to be the important scaffold for maintaining selective on-off sensor capacity that renders the compound a selective Iron (III) binding probe. Moreover, for the first time, fluorescence cellular imaging studies concomitant to cytotoxicity assays with the title compounds were also performed and the results displayed the cell-penetrative, safe, and fluorescent detectable characteristics of the compounds in neuroblastoma and glioblastoma cells through servings as intracellular Iron (III) on-off sensors.
